Monograph Details
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Infections & Infestations
> Viral infections
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APTIVUS ORAL SOLUTION |
| Manufacturer |
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Boehringer Ingelheim Pharmaceuticals |
| Legal Classification |
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Rx
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| Pharmacological Class |
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HIV-1 protease inhibitor. |
| Generic Name |
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Tipranavir 100mg/mL; contains Vit.E 116 IU/mL; buttermint-butter toffee flavor. |
| Also |
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• APTIVUS
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| Indications |
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HIV-1 infection in treatment-experienced patients or in those with HIV strains resistant to multiple protease inhibitors (PIs) in combination with ritonavir. |
| Children |
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<2 years: not recommended. Use soln if unable to swallow caps. 2–18 years: Tipranavir 14mg/kg + ritonavir 6mg/kg twice daily; max tipranavir 500mg + ritonavir 200mg twice daily. May consider reducing dose to tipranavir 12mg/kg + ritonavir 5mg/kg twice daily if intolerance or toxicity occurs provided their virus is not resistant to multiple PIs. |
| Adults |
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Swallow caps whole. Tipranavir 500mg + ritonavir 200mg twice daily. |
| Contraindications |
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Moderate to severe hepatic insufficiency (Child-Pugh B–C). Concomitant potent CYP3A inducers or substrates (eg, amiodarone, bepridil, flecainide, propafenone, quinidine, rifampin, ergots, cisapride, St. John's wort, lovastatin, simvastatin, pimozide, oral midazolam, triazolam). |
| Precautions |
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Not for use in treatment-naive patients. Sulfa allergy. Mild hepatic impairment (Child-Pugh A). Hepatitis. Monitor lipids, liver function (baseline and periodically); discontinue if asymptomatic increase in AST/ALT >10xULN, or AST/ALT 5–10xULN and total bilirubin >2.5xULN. Diabetes. Risk of increased bleeding. Hemophilia: monitor for spontaneous bleeding. Pregnancy (Cat.C). Nursing mothers: not recommended. |
| Interactions |
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See Contraindications. Concomitant fluticasone, amprenavir, lopinavir, saquinavir, or fluconazole, ketoconazole, itraconazole ≥200mg/day: not recommended. Avoid metronidazole, disulfiram. May be synergistic with enfuvirtide. Potentiates PDE5 inhibitors (eg, sildenafil, tadalafil, vardenafil), trazodone, desipramine; reduce dose: see literature. Reduce rifabutin dose by 75%. Antagonizes estrogens (use non-hormonal contraceptives), methadone, valproic acid, omeprazole. Antagonized by carbamazepine, phenobarbital, phenytoin. Potentiates atorvastatin, rosuvastatin: use lowest possible dose. Monitor hypoglycemics, immunosuppressants, tricyclics, SSRIs, warfarin, drugs that affect or are affected by CYP3A4 (eg, azole antifungals, calcium channel blockers, clarithromycin, NNRTIs, PIs, statins). Increased risk of bleeding with concomitant anticoagulants, antiplatelet agents, high-dose Vit.E. Separate dosing of didanosine, antacids. Oral soln: avoid high-dose Vit.E supplements. |
| Adverse Reactions |
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GI upset, abdominal pain, pyrexia, fatigue, headache, rash (discontinue if severe), fat redistribution, severe liver disease, hepatitis (discontinue if symptomatic), hypertriglyceridemia, hyperlipidemia, hyperglycemia, immune reconstitution syndrome, intracranial hemorrhage (may be fatal), others; children: also cough. |
| Extra Text |
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Note: Register pregnant patients exposed to tipranavir by calling (800) 258-4263. |
| How Supplied |
Caps—120
Soln—95mL (w. dispensing syringe) |
| Additional Resources |
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• Related Prescribing Note |
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